ACY-775

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Chemical Structure| 1375466-18-4 同义名 : -
CAS号 : 1375466-18-4
货号 : A725076
分子式 : C17H19FN4O2
纯度 : 99%+
分子量 : 330.36
MDL号 : MFCD30533691
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(75.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 HDAC6 (histone deacetylase 6) is a structurally and functionally unique class Iib isoform localized almost exclusively to the cytoplasm. HDAC6 loss of function results in an antidepressant-like phenotype. ACE-775 is a potent and selective HDAC6 inhibitor with an IC50 value of 7.5 nM. In RN46A-B14 cells treated with ACY-775 (2.5 μM) for 4 hours, there was an increase in the acetylated (lysine 40) fraction of α-tubulin. ACY-775 rapidly distribute to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues. In wild-type mice, ACY-775 (50 mg/kg; 24 h, 4 h, and 30 min) caused significant increases in α-tubulin acetylation in all tested brain regions: cortex, hippocampus and cerebellum and stimulated mouse exploratory behaviors in novel environments[3].
作用机制 Activity of ACY-775 is fully explained by inhibition of the C terminal catalytic domain of HDAC6[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.03mL

0.61mL

0.30mL

15.14mL

3.03mL

1.51mL

30.27mL

6.05mL

3.03mL
参考文献

[1]Veronick Benoy, et al. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr; 14(2): 417-428.

[2]Jeanine Jochems et al. Antidepressant-Like Properties of Novel HDAC6-Selective Inhibitors with Improved Brain Bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2): 389-400.

[3]Jochems J, et al. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400